Page last updated: 2024-10-15

amg 221

Description

AMG 221: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID135565424
CHEMBL ID1085107
SCHEMBL ID10284762
SCHEMBL ID23798787
MeSH IDM0537202

Synonyms (20)

Synonym
CHEMBL1085107 ,
amg-221
bdbm50319665
(s)-2-((1s,2s,4r)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5h)-one
4(5h)-thiazolone, 2-((1s,2s,4r)-bicyclo(2.2.1)hept-2-ylamino)-5-methyl-5-(1-methylethyl)-, (5s)-
2t929w7ag8 ,
1095565-81-3
unii-2t929w7ag8
amg 221
948044-21-1
bvt-83370
SCHEMBL10284762
Q27255579
(5s)-2-[[(1s,2s,4r)-2-bicyclo[2.2.1]heptanyl]imino]-5-methyl-5-propan-2-yl-1,3-thiazolidin-4-one
(5s)-2-[[(1s,2s,4r)-2-bicyclo[2.2.1]heptanyl]amino]-5-methyl-5-propan-2-yl-1,3-thiazol-4-one
cid 25207668
HY-10555
CS-0002637
SCHEMBL23798787
AKOS040747810

Research Excerpts

Overview

AMG 221 is a potent, small molecule inhibitor of 11β-HSD1.

ExcerptReference
"AMG 221 is a potent, small molecule inhibitor of 11β-HSD1."( Population pharmacokinetic/pharmacodynamic model of subcutaneous adipose 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) activity after oral administration of AMG 221, a selective 11β-HSD1 inhibitor.
Akrami, A; Bautista, E; Daniels, O; Emery, MG; Gastonguay, MR; Gibbs, JP; Gibbs, MA; McCaffery, I; Paweletz, K; Perfetti, R; Rossi, J; Smith, B; Wang, M, 2011
)

Toxicity

ExcerptReference
" Rat and dog area under the plasma concentration time curve (AUC) exposures to M1 at preclinical no observable adverse effect level (NOAEL) doses were 2-42-fold higher than human, indicating M1 was not a disproportionate metabolite, as defined by International Committee on Harmonization (ICH) M3(R2) guidance."( Activity-based exposure comparisons among humans and nonclinical safety testing species in an extensively metabolized drug candidate.
Akrami, A; Deane, MR; Emery, MG; Hickman, D; Skiles, GL; Slatter, JG; Subramanian, R; Zhang, X; Zhu, X, 2013
)

Bioavailability

ExcerptReference
" A catheterized rat model was used to define the intestinal and hepatic components of oral bioavailability for an 11β-HSD1 inhibitor, AMG 221."( Intestinal and hepatic first-pass extraction of the 11β-HSD1 inhibitor AMG 221 in rats with chronic vascular catheters.
Amore, BM; Emery, MG; Gao, Q; Greg Slatter, J; Hickman, D; Kimura, RE; Nam, J; Zhang, X, 2014
)
" After further profiling, we determined that metabolite 2 was equipotent to 1 on human 11β-HSD1 and had lower in vivo clearance and higher bioavailability in rat and mouse."( Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
Chen, M; Chow, D; Emery, MG; Fotsch, C; Hale, C; Komorowski, R; Li, A; St Jean, DJ; Subramanian, R; Véniant, M; Wang, M; Yuan, CC; Zhang, X, 2011
)

Dosage Studied

ExcerptReference
"1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221) in rats was dosed at 2 mg/kg."( Regiospecific and stereospecific triangulation of the structures of metabolites formed by sequential metabolism at multiple prochiral centers.
Davis, JA; Deane, MR; Emery, MG; Greene, RJ; Slatter, JG; Subramanian, R, 2012
)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (9)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Glucocorticoid receptorHomo sapiens (human)IC50 (µMol)10.00000.00000.495310.0000AID483785
Cytochrome P450 1A2Homo sapiens (human)IC50 (µMol)15.00000.00011.774010.0000AID483804
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)15.00000.00011.753610.0000AID483802
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)15.00000.00002.015110.0000AID483803
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)15.00000.00002.800510.0000AID483805
Corticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)IC50 (µMol)3.34010.00411.066710.0000AID483782; AID483784; AID657806
Corticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)Ki0.01280.00100.10010.6200AID483781; AID657805
Cytochrome P450 2C19Homo sapiens (human)IC50 (µMol)15.00000.00002.398310.0000AID483806
Corticosteroid 11-beta-dehydrogenase isozyme 1Mus musculus (house mouse)Ki0.07080.01000.22940.7500AID657807
Corticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)IC50 (µMol)10.00000.00040.63676.4300AID483783
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (81)

Processvia Protein(s)Taxonomy
negative regulation of transcription by RNA polymerase IIGlucocorticoid receptorHomo sapiens (human)
regulation of gluconeogenesisGlucocorticoid receptorHomo sapiens (human)
chromatin organizationGlucocorticoid receptorHomo sapiens (human)
regulation of DNA-templated transcriptionGlucocorticoid receptorHomo sapiens (human)
apoptotic processGlucocorticoid receptorHomo sapiens (human)
chromosome segregationGlucocorticoid receptorHomo sapiens (human)
signal transductionGlucocorticoid receptorHomo sapiens (human)
glucocorticoid metabolic processGlucocorticoid receptorHomo sapiens (human)
gene expressionGlucocorticoid receptorHomo sapiens (human)
microglia differentiationGlucocorticoid receptorHomo sapiens (human)
adrenal gland developmentGlucocorticoid receptorHomo sapiens (human)
regulation of glucocorticoid biosynthetic processGlucocorticoid receptorHomo sapiens (human)
synaptic transmission, glutamatergicGlucocorticoid receptorHomo sapiens (human)
maternal behaviorGlucocorticoid receptorHomo sapiens (human)
intracellular glucocorticoid receptor signaling pathwayGlucocorticoid receptorHomo sapiens (human)
glucocorticoid mediated signaling pathwayGlucocorticoid receptorHomo sapiens (human)
positive regulation of neuron apoptotic processGlucocorticoid receptorHomo sapiens (human)
negative regulation of DNA-templated transcriptionGlucocorticoid receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIGlucocorticoid receptorHomo sapiens (human)
astrocyte differentiationGlucocorticoid receptorHomo sapiens (human)
cell divisionGlucocorticoid receptorHomo sapiens (human)
mammary gland duct morphogenesisGlucocorticoid receptorHomo sapiens (human)
motor behaviorGlucocorticoid receptorHomo sapiens (human)
cellular response to steroid hormone stimulusGlucocorticoid receptorHomo sapiens (human)
cellular response to glucocorticoid stimulusGlucocorticoid receptorHomo sapiens (human)
cellular response to dexamethasone stimulusGlucocorticoid receptorHomo sapiens (human)
cellular response to transforming growth factor beta stimulusGlucocorticoid receptorHomo sapiens (human)
neuroinflammatory responseGlucocorticoid receptorHomo sapiens (human)
positive regulation of miRNA transcriptionGlucocorticoid receptorHomo sapiens (human)
intracellular steroid hormone receptor signaling pathwayGlucocorticoid receptorHomo sapiens (human)
regulation of transcription by RNA polymerase IIGlucocorticoid receptorHomo sapiens (human)
steroid catabolic processCytochrome P450 1A2Homo sapiens (human)
porphyrin-containing compound metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 1A2Homo sapiens (human)
cholesterol metabolic processCytochrome P450 1A2Homo sapiens (human)
estrogen metabolic processCytochrome P450 1A2Homo sapiens (human)
toxin biosynthetic processCytochrome P450 1A2Homo sapiens (human)
post-embryonic developmentCytochrome P450 1A2Homo sapiens (human)
alkaloid metabolic processCytochrome P450 1A2Homo sapiens (human)
regulation of gene expressionCytochrome P450 1A2Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 1A2Homo sapiens (human)
dibenzo-p-dioxin metabolic processCytochrome P450 1A2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lung developmentCytochrome P450 1A2Homo sapiens (human)
methylationCytochrome P450 1A2Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 1A2Homo sapiens (human)
retinol metabolic processCytochrome P450 1A2Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 1A2Homo sapiens (human)
cellular respirationCytochrome P450 1A2Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 1A2Homo sapiens (human)
hydrogen peroxide biosynthetic processCytochrome P450 1A2Homo sapiens (human)
oxidative demethylationCytochrome P450 1A2Homo sapiens (human)
cellular response to cadmium ionCytochrome P450 1A2Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
lung developmentCorticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)
steroid catabolic processCorticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)
long-chain fatty acid metabolic processCytochrome P450 2C19Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C19Homo sapiens (human)
steroid metabolic processCytochrome P450 2C19Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C19Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C19Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
response to hypoxiaCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
regulation of blood volume by renal aldosteroneCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
female pregnancyCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
response to xenobiotic stimulusCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
response to foodCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
response to insulinCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
cortisol metabolic processCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
response to glucocorticoidCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
glucocorticoid metabolic processCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (59)

Processvia Protein(s)Taxonomy
RNA polymerase II transcription regulatory region sequence-specific DNA bindingGlucocorticoid receptorHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingGlucocorticoid receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificGlucocorticoid receptorHomo sapiens (human)
core promoter sequence-specific DNA bindingGlucocorticoid receptorHomo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificGlucocorticoid receptorHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificGlucocorticoid receptorHomo sapiens (human)
DNA-binding transcription factor activityGlucocorticoid receptorHomo sapiens (human)
RNA bindingGlucocorticoid receptorHomo sapiens (human)
nuclear receptor activityGlucocorticoid receptorHomo sapiens (human)
nuclear glucocorticoid receptor activityGlucocorticoid receptorHomo sapiens (human)
steroid bindingGlucocorticoid receptorHomo sapiens (human)
protein bindingGlucocorticoid receptorHomo sapiens (human)
zinc ion bindingGlucocorticoid receptorHomo sapiens (human)
TBP-class protein bindingGlucocorticoid receptorHomo sapiens (human)
protein kinase bindingGlucocorticoid receptorHomo sapiens (human)
identical protein bindingGlucocorticoid receptorHomo sapiens (human)
Hsp90 protein bindingGlucocorticoid receptorHomo sapiens (human)
steroid hormone bindingGlucocorticoid receptorHomo sapiens (human)
sequence-specific double-stranded DNA bindingGlucocorticoid receptorHomo sapiens (human)
estrogen response element bindingGlucocorticoid receptorHomo sapiens (human)
monooxygenase activityCytochrome P450 1A2Homo sapiens (human)
iron ion bindingCytochrome P450 1A2Homo sapiens (human)
protein bindingCytochrome P450 1A2Homo sapiens (human)
electron transfer activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 1A2Homo sapiens (human)
enzyme bindingCytochrome P450 1A2Homo sapiens (human)
heme bindingCytochrome P450 1A2Homo sapiens (human)
demethylase activityCytochrome P450 1A2Homo sapiens (human)
caffeine oxidase activityCytochrome P450 1A2Homo sapiens (human)
aromatase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityCytochrome P450 1A2Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
protein homodimerization activityCorticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)
7-beta-hydroxysteroid dehydrogenase (NADP+) activityCorticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)
NADP bindingCorticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)
11-beta-hydroxysteroid dehydrogenase (NADP+) activityCorticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)
cortisol dehydrogenase activityCorticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)
steroid bindingCorticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)
monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
iron ion bindingCytochrome P450 2C19Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxygen bindingCytochrome P450 2C19Homo sapiens (human)
enzyme bindingCytochrome P450 2C19Homo sapiens (human)
heme bindingCytochrome P450 2C19Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
aromatase activityCytochrome P450 2C19Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C19Homo sapiens (human)
steroid bindingCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
NAD bindingCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
11-beta-hydroxysteroid dehydrogenase (NAD+) activityCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (17)

Processvia Protein(s)Taxonomy
nucleusGlucocorticoid receptorHomo sapiens (human)
nucleusGlucocorticoid receptorHomo sapiens (human)
nucleoplasmGlucocorticoid receptorHomo sapiens (human)
cytoplasmGlucocorticoid receptorHomo sapiens (human)
mitochondrial matrixGlucocorticoid receptorHomo sapiens (human)
centrosomeGlucocorticoid receptorHomo sapiens (human)
spindleGlucocorticoid receptorHomo sapiens (human)
cytosolGlucocorticoid receptorHomo sapiens (human)
membraneGlucocorticoid receptorHomo sapiens (human)
nuclear speckGlucocorticoid receptorHomo sapiens (human)
synapseGlucocorticoid receptorHomo sapiens (human)
chromatinGlucocorticoid receptorHomo sapiens (human)
protein-containing complexGlucocorticoid receptorHomo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
endoplasmic reticulum membraneCorticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)
membraneCorticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)
endoplasmic reticulum membraneCorticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)
intracellular membrane-bounded organelleCorticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C19Homo sapiens (human)
plasma membraneCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
cytoplasmCytochrome P450 2C19Homo sapiens (human)
endoplasmic reticulum membraneCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
intracellular membrane-bounded organelleCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
intracellular membrane-bounded organelleCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (61)

Assay IDTitleYearJournalArticle
AID483790Clearance in Sprague-Dawley rat at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483800Terminal half life in cynomolgus monkey at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID657810Terminal half life in Sprague-Dawley rat at 2 mg/kg, iv and 10 mg/kg, po2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID657844Plasma protein binding in po dosed mouse after 4 hrs2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID1151435Inhibition of adipose tissue-derived 11beta-HSD1 (unknown origin) assessed as concentration required for maximal inhibition2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1).
AID483802Inhibition of CYP3A42010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483804Inhibition of CYP1A22010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID657808Clearance in Sprague-Dawley rat at 2 mg/kg, iv and 10 mg/kg, po2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID483806Inhibition of CYP2C192010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483808Ex vivo inhibition of 11beta-HSD1 in high fat diet-fed C57BL/6 mouse inguinal fat at 5 mg/kg, po measured at 4 hrs by ELISA2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483792Terminal half life in Sprague-Dawley rat at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID657826Ratio of drug level in adipose tissue fat to plasma of mouse at 50 mg/kg, po2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID483807Metabolic stability in liver microsomes2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483788Terminal half life in CD1 mouse at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID657812Oral bioavailability in Sprague-Dawley rat at 10 mg/kg2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID1151434Inhibition of adipose tissue-derived 11beta-HSD1 (unknown origin)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1).
AID483787Volume of distribution at steady state in CD1 mouse at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID1071798Inhibition of 11beta-HSD1 in mouse liver microsomes using cortisone as substrate after 2 hrs by HTRF assay2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
3-Amino-N-adamantyl-3-methylbutanamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitor.
AID657805Inhibition of human 11beta-HSD1 expressed in Escherichia coli using [3H]cortisone as substrate by scintillation proximity assay2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID483812Ex vivo inhibition of 11beta-HSD1 in high fat diet-fed C57BL/6 mouse inguinal fat at 15 mg/kg, po measured at 8 hrs by ELISA2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID657815Half life in CD1 mouse at 2 mg/kg, iv and 10 mg/kg, po2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID483821Antiobesity activity in diet-induced obese mouse assessed as decrease in body weight at 5 mg/kg administered QD via high fat-diet for 13 days measured after day 132010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID1218573Oral bioavailability in rat2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Regiospecific and stereospecific triangulation of the structures of metabolites formed by sequential metabolism at multiple prochiral centers.
AID657813Clearance in CD1 mouse at 2 mg/kg, iv and 10 mg/kg, po2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID483803Inhibition of CYP2D62010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID1218574Volume of distribution at steady state in rat2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Regiospecific and stereospecific triangulation of the structures of metabolites formed by sequential metabolism at multiple prochiral centers.
AID483801Bioavailability in cynomolgus monkey at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483794Clearance in Beagle dog at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483797Bioavailability in Beagle dog at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483805Inhibition of CYP2C92010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483789Bioavailability in CD1 mouse at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483799Volume of distribution at steady state in cynomolgus monkey at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483795Volume of distribution at steady state in Beagle dog at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID1218572Plasma protein binding in rat2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Regiospecific and stereospecific triangulation of the structures of metabolites formed by sequential metabolism at multiple prochiral centers.
AID657806Inhibition of human 11beta-HSD1 expressed in CHO cells2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID1218571Plasma protein binding in human2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Regiospecific and stereospecific triangulation of the structures of metabolites formed by sequential metabolism at multiple prochiral centers.
AID657843Free plasma concentration in po dosed mouse after 4 hrs2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID483815Antidiabetic activity in diet-induced obese mouse assessed as decrease in plasma insulin level at 25 to 50 mg/kg, po administered via gavage BID for 13 days measured after day 13 by glucose tolerance test2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483818Antidiabetic activity in diet-induced obese mouse assessed as mild improvement of glucose tolerance at 25 to 50 mg/kg, ip BID for 13 days measured on day 14 after 12 hrs of fasting by glucose tolerance test2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483782Displacement of [3H]-cortisone human 17beta-HSD1 expressed in HEK293 cells after 30 mins by scintillation proximity assay2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID657816Oral bioavailability in CD1 mouse at 10 mg/kg2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID483785Inhibition of glucocorticoid receptor2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483813Ex vivo inhibition of 11beta-HSD1 in high fat diet-fed C57BL/6 mouse inguinal fat at 50 mg/kg, po measured at 8 hrs by ELISA2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483784Inhibition of 11beta-HSD12010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483810Ex vivo inhibition of 11beta-HSD1 in high fat diet-fed C57BL/6 mouse inguinal fat at 50 mg/kg, po measured at 4 hrs by ELISA2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID657807Inhibition of mouse 11beta-HSD1 expressed in Escherichia coli using [3H]cortisone as substrate by scintillation proximity assay2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID483820Antiobesity activity in po dosed diet-induced obese mouse assessed as decrease in body weight administered via gavage BID for 13 days measured after day 132010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483793Bioavailability in Sprague-Dawley rat at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483781Displacement of [3H]-cortisone human 17beta-HSD1 expressed in Escherichia coli after 30 mins by scintillation proximity assay2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483798Clearance in cynomolgus monkey at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID657809Volume of distribution at steady state in Sprague-Dawley rat at 2 mg/kg, iv and 10 mg/kg, po2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID483783Inhibition of 11beta-HSD22010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID1218575Clearance in iv dosed rat2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Regiospecific and stereospecific triangulation of the structures of metabolites formed by sequential metabolism at multiple prochiral centers.
AID483791Volume of distribution at steady state in Sprague-Dawley rat at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID657814Volume of distribution at steady state in CD1 mouse at 2 mg/kg, iv and 10 mg/kg, po2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID483811Ex vivo inhibition of 11beta-HSD1 in high fat diet-fed C57BL/6 mouse inguinal fat at 5 mg/kg, po measured at 8 hrs by ELISA2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483814Antidiabetic activity in diet-induced obese mouse assessed as decrease in fed blood glucose level at 25 to 50 mg/kg, po administered via gavage BID for 13 days measured after day 13 by glucose tolerance test2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483786Clearance in CD1 mouse at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483809Ex vivo inhibition of 11beta-HSD1 in high fat diet-fed C57BL/6 mouse inguinal fat at 15 mg/kg, po measured at 4 hrs by ELISA2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID1071799Inhibition of 11beta-HSD1 in human liver microsomes using cortisone as substrate after 2 hrs by HTRF assay2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
3-Amino-N-adamantyl-3-methylbutanamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitor.
AID483796Terminal half life in Beagle dog at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (11.11)29.6817
2010's8 (88.89)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (11.11%)5.53%
Reviews1 (11.11%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (77.78%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]